[(2R)-1-[(2S)-2-氨基-3-甲基丁酰基]吡咯烷-2-基]硼酸
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- CAS号:
- 149682-77-9
- 英文名:
- VAL-BORO-PRO
- 英文别名:
- Pt 100;TALABOSTA;talabostat;VAL-BORO-PRO;Unii-kz1o2sh88z;Talabostat (PT100);Adrafinil Impurity 5;Talabostat (Val-boroPro, PT-100);PT-100;VALBOROPRO;VAL-BOROPRO;PT100;PT 100;((R)-1-((S)-2-Amino-3-methylbutanoyl)pyrrolidin-2-yl)boronic acid
- 中文名:
- [(2R)-1-[(2S)-2-氨基-3-甲基丁酰基]吡咯烷-2-基]硼酸
- 中文别名:
- [(2R)-1-[(2S)-2-氨基-3-甲基丁酰基]吡咯烷-2-基]硼酸;Talabostat (PT-100;ValboroPro;Val-boroPro;PT100;PT 100)
- CBNumber:
- CB01011676
- 分子式:
- C9H19BN2O3
- 分子量:
- 214.07
- MOL File:
- 149682-77-9.mol
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[(2R)-1-[(2S)-2-氨基-3-甲基丁酰基]吡咯烷-2-基]硼酸化学性质
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沸点:
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421.4±55.0 °C(Predicted)
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密度:
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1.15
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储存条件:
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Store at -20°C
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溶解度:
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DMSO : ≥ 40 mg/mL (186.85 mM)
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酸度系数(pKa):
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9.71±0.20(Predicted)
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[(2R)-1-[(2S)-2-氨基-3-甲基丁酰基]吡咯烷-2-基]硼酸性质、用途与生产工艺
Talabostat (Val-boroPro; PT100) 是一种口服活性和非选择性的二肽基肽酶 IV (DPP-IV) 抑制剂 (IC50 < 4 nM; Ki = 0.18 nM) 和成纤维细胞活化蛋白 (FAP) 的第一个临床抑制剂 (IC50 = 560 nM)，抑制 DPP8/9 (IC50 = 4/11 nM; Ki = 1.5/0.76 nM)，静息细胞脯氨酸二肽酶 (QPP) (IC50 = 310 nM)、DPP2 和一些其他 DASH 家族酶。具有抗肿瘤和造血刺激活性 。
IC50: < 4 nM (DPP-IV), 4/11 nM (DPP8/9), 310 nM (QPP), 560 nM (FAP)
Ki: 0.18 nM (DPP-IV), 1.5/0.76 nM (DPP8/9)
By cleaving N-terminal Xaa-Pro or Xaa-Ala residues, Talabostat (Val-boroPro) inhibits dipeptidyl peptidases, such as FAP, resulting in the stimulation of cytokine and chemokine production and specific T-cell immunity and T-cell dependent activity.
Talabostat (Val-boroPro) competitively inhibits the dipeptidyl peptidase (DPP) activity of FAP and CD26/DPP-IV, and there is a high-affinity interaction with the catalytic site.
Talabostat (Val-boroPro; PT100) can stimulate immune responses against tumors involving both the innate and adaptive branches of the immune system.In WEHI 164 fibrosarcoma and EL4 and A20/2J lymphoma models, Talabostat (Val-boroPro) causes regression and rejection of tumors. The antitumor effect appears to involve tumor-specific CTL and protective immunological memory.Talabostat (Val-boroPro) treatment of WEHI 164-inoculated mice increases mRNA expression of cytokines and chemokines known to promote T-cell priming and chemoattraction of T cells and innate effector cells.
[(2R)-1-[(2S)-2-氨基-3-甲基丁酰基]吡咯烷-2-基]硼酸
上下游产品信息
上游原料
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[(2R)-1-[(2S)-2-氨基-3-甲基丁酰基]吡咯烷-2-基]硼酸
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149682-77-9, [(2R)-1-[(2S)-2-氨基-3-甲基丁酰基]吡咯烷-2-基]硼酸 相关搜索:
- 抑制剂
- 对照品
- 放射显影多肽产品
- C9H19BN2O3
- Talabostat (PT-100;ValboroPro;Val-boroPro;PT100;PT 100)
- [(2R)-1-[(2S)-2-氨基-3-甲基丁酰基]吡咯烷-2-基]硼酸
- 149682-77-9
- Adrafinil Impurity 5
- ((R)-1-((S)-2-Amino-3-methylbutanoyl)pyrrolidin-2-yl)boronic acid
- PT-100;VALBOROPRO;VAL-BOROPRO;PT100;PT 100
- [(2R)-1-[(2S)-2-amino-3-methylbutanoyl]pyrrolidin-2-yl]boronic acid
- Talabostat/ Boronic acid, [(2R)-1-[(2S)-2-aMino-3-Methyl-1-oxobutyl]-2-pyrrolidinyl]-
- Talabostat (Val-boroPro, PT-100)
- TALABOSTA
- [(2R)-1-[(2S)-2-Amino-3-methyl-1-oxobutyl]-2-pyrrolidinyl]boronic acid
- Talabostat (PT100)
- VAL-BORO-PRO
- Unii-kz1o2sh88z
- Pt 100
- Boronic acid, (1-(2-amino-3-methyl-1-oxobutyl)-2-pyrrolidinyl)-, (R-(R*,S*))-
- Boronic acid, ((2R)-1-((2S)-2-amino-3-methyl-1-oxobutyl)-2-pyrrolidinyl)-
- talabostat